That Grapefruit and Medicines can Possibly be a Fatal Combination

eating or drinking grapefruit juice while taking medication can be very dangerous. Orally ingested medicines have an absorption rate under 100% — sometimes only 25% of the active ingredient in the drug makes it into your blood stream. This is accounted for when prescribing the right dose. Furanocoumarins found in grapefruit and some other fruits can increase absorption and possibly lead to fatal overdoses. This doesn’t happen for all medicines but better to be on the safe side and Always ask your doctor.

Some fruit juices and fruits can interact with numerous drugs, in many cases causing adverse effects. The effect was first discovered accidentally, when a test of drug interactions with alcohol used grapefruit juice to hide the taste of the ethanol.

The effect is most studied with grapefruit and grapefruit juice, but similar effects have been observed with certain other citrus fruits. One medical review advises patients to avoid all citrus juices until further research clarifies the risks. Effects have been observed with apple juice, but their clinical significance is not yet known.

One whole grapefruit, or a small glass (200 mL (6.8 US fl oz)) of grapefruit juice, can cause drug overdose toxicity. Fruit consumed three days before the medicine can still have an effect. The relative risks of different types of citrus fruit have not been systematically studied. Affected drugs typically have an auxiliary label saying “Do not take with grapefruit” on the container, and the interaction is elaborated upon in the package insert. People are also advised to ask their physician or pharmacist about drug interactions.

The effects are caused by furanocoumarins (and, to a lesser extent, flavonoids). These chemicals inhibit key drug metabolizing enzymes, such as cytochrome P450 3A4 (CYP3A4). CYP3A4 is a metabolizing enzyme for almost 50% of drugs, and is found in the liver and small intestinal epithelial cells. As a result, many drugs are affected. Inhibition of enzymes can have two different effects, depending on whether the drug is either

In the first instance, inhibition of drug-metabolizing enzymes results in elevated concentrations of an active drug in the body, which may cause adverse effects. Conversely, if the medication is a prodrug, it needs to be metabolised to be converted to the active drug. Compromising its metabolism lowers concentrations of the active drug, reducing its therapeutic effect, and risking therapeutic failure.

The effect of grapefruit juice with regard to drug absorption was originally discovered in 1989. The first published clinical report on grapefruit drug interactions was in 1991 in The Lancet entitled “Interactions of Citrus Juices with Felodipine and Nifedipine.”However, the effect only became well-publicized after being responsible for a number of adverse interactions with various medications.

Citrus fruits may contain a number of polyphenol compounds, including the flavonoid naringin and furanocoumarins (such as bergamottin, bergapten, and bergaptol).These are natural chemicals. They may be present in all forms of the fruit, including freshly squeezed juice, frozen concentrate, and whole fruit.

Grapefruit, Seville oranges, bergamot, and possibly other citrus also contain large amounts of naringin. It can take up to 72 hours before the effects of the naringin on the CYP3A4 enzyme are seen. This is problematic as a 4-ounce (110 g) portion of grapefruit contains enough naringin to inhibit the metabolism of substrates of CYP3A4. Naringin is a flavonoid which contributes to the bitter flavour of grapefruit.

Furanocoumarins seem to have a stronger effect than naringin under some circumstances.

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